21^st International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems March 11-12, 2020 Rome, Italy

Biography:

Stefania Petralito received the Laurea degree in pharmacy, the Ph.D. degree in Pharmaceutical Science and a  Postgraduate Diploma in Hospital Pharmacy from the Sapienza University of Rome, in 1997, 2000 and 2003 respectively. In 2005, she joined the Department of Drug Chemistry and Technologies, Sapienza, as a researcher. Her current research interests include preparation and characterization of vesicular systems as drug delivery systems. She is a member of the Controlled Release Society Italian Chapter (C.R.S.), of the Società Chimica Italiana (SCI)-Division of Pharmaceutic Technology, of the Association of Italian Doctors, and Researchers of Pharmaceutical Technology and Legislation (A.D.R.I.T.E.L.F.).

Abstract:

Magnetic nanoparticles with superparamagnetic properties have attracted increased attention for applications in biomedicine, as they exhibit a strong magnetization only when an external magnetic field is applied. Magnetoliposomes (MLs) are the combination of liposomes with encapsulated magnetic nanoparticles. These hybrid nanocarriers have been showing significant biomedical application possibilities. However, it is essential that nanoparticles exhibit superparamagnetism, this causes nanoparticles to become susceptible to strong magnetization. When the magnetic field is applied, they orient toward this field, but do not retain permanent magnetization in the absence of magnetic field. The magnetic properties of super paramagnetic iron oxide nanoparticles (SPIONs)-based magnetoliposomes allow for alternative therapies through magnetically controlled drug delivery and hyperthermia. In this way they can be viewed as trigger-responsive carriers as they have the potential to act as "remote switch" that can turn on or off the effects of the therapeutics, based on the presence or absence of the stimulus. Recently, a pilot study has demonstrated the feasibility of smart controlled delivery through a magnetic field with intensity significantly lower than the ones usually reported in literature. In this way, a controlled release has been obtained through a magneto-nanomechanical approach without any macroscopic temperature increase. Specifically, signals generated by non-thermal alternating magnetic fields (AMFs) or non-thermal pulsed electromagnetic fields (PEMFs) were applied to high-transition temperature magnetoliposomes (high-Tm MLs) entrapping hydrophilic SPIONs, proving to be interesting and promising stimuli-controlled drug delivery systems

Biography:

Marta Ruano is a Chemical Engineer who obtained a PhD from the Physical-Chemistry Department of University Complutense of Madrid with the thesis entitled Fabrication of liposomes and polymeric microcapsules. She has 5 years expertise in drug delivery systems for food, cosmetics, and nutraceuticals: liposomes, polymeric micro and nano microparticles with different actives after years dedicated to this research in a R&D technology center. In 2018, she started the KTP project in Glasgow where AB Vista and the University of Strathclyde are involved. The aim of this project is the development of novel nano-delivery systems incorporating bioactive lipids and peptides in animal food formulation with effective antimicrobial stewardship to reduce antibiotic resistance in the food chain.

Abstract:

Background: Cubosomes are cubic lyotropic Liquid Crystalline structures consisting of polar lipids, such as glycerol monooleate (GMO) or glycerol monolaurate (GML) that provide the capability of carrying both hydrophilic and lipophilic compounds1-3. The most straightforward method of producing cubic phase particles is the agitation of both phases (oil and water) with a magnetic stirrer resulting in a coarse dispersion. This produces a polydisperse and unstable solution. Further post-manufacture modifications are required to control dispersity and size: ultrasonication5, homogenisation6, and microfluidics7.

Aims: The aim of the present study was to formulate cubosomes (see Figure 1)4 in the presence of ethanol (hydrotrope) prepared comparing the three post-manufacture methods.

Methods: Three samples were prepared using GMO and GML dissolved in ethanol (oil phase) and the surfactant (F127) dissolved in water (water phase). One sample was sonicated for 5 minutes using 30-40% of the maximum power. The second sample was homogenised for 10 minutes at 8000 rpm. The third sample was prepared using a Neonano device from Neofluidics for 1 minute. The samples were examined by Scanning Electron Microscopy to determine if cubosomes had been formed, and evaluated by Dynamic Light Scattering (DLS) for measurement of particle size and Zeta potential using a Zetasizer Nano ZS90 system to provide a comparison of average droplet size and polydispersity index between all the samples and the measurements of zeta potential showed which method provides better colloidal stability during storage for three months at 4, 25 and 37ºC.

Results: The dispersions examined under Scanning Electronic Microscope showed non-aggregated particles confirming the nanoparticle formation for all three methods. The sample produced by microfluidics showed low polydispersity with no variation of the zeta potential over three months.

Conclusion: Microfluidics avoids the heat gradient and it reduces the manufacture time with high reproducibility

Biography:

Kármen Szabó is a doctoral candidate at the Inorganic and Analytical Chemistry Department of the University of Debrecen (Debrecen, Hungary). She is a member of a biochemical research group, which primarily focuses on the investigation and inhibition of carbohydrate-active enzymes (glycoenzymes). Kármen has dealt with the examination of natural and synthetic compounds that could be applied as medicaments for the treatment and/or the prevention of type 2 diabetes mellitus and its complications. She has recently been concerned with the identification and interpretation of drug promiscuity, especially for known and potential anti-diabetic agents. Drug promiscuity, which can be defined as the outstanding inhibitory effect of a compound on various unrelated target enzymes, can lead to financial losses for pharmaceutical industry if it is recognized too late. Therefore, her work can be feasible for eliminating these promiscuous inhibitors even at an early stage in drug development.

Abstract:

Statement of the Problem: According to the International Diabetes Federation (IDF), type 2 diabetes mellitus as well as its complications caused the death of about 4.2 million adults in 20191. Although many effective drugs are currently available, their diverse and often severe side effects require the development of new, safer alternative therapies2. The inhibition of aldose reductase (AR) enzyme can ease or even prevent the development of such longterm complications of diabetes as kidney failure, blindness, or cardiovascular diseases. 4-thiazolidinone derivatives were designed as potential AR-inhibitors3; however, the promiscuous nature of these compounds must be investigated before applying them as drugs.

Methodology & Theoretical Orientation: Our research aimed to determine whether these 4-thiazolidinone derivatives meet the criteria of promiscuity found in the literature. These criteria are as follows: (1) time-dependence, (2) sensitivity both to the change in enzyme concentration as well as to the presence of a detergent, and (3) a considerable inhibitory effect on target enzymes with significantly different mechanisms and/or functions4-5. Activity measurements were carried out spectrophotometrically, using a chromophore-containing substrate and porcine pancreatic α-amylase as enzyme. Since aggregation can be a reason of promiscuity, in the case of those inhibitors that had turned to be promiscuous, I also examined their aggregation-tendency by HPLC.

Findings: Three out of the seven tested inhibitors found to be promiscuous. In these cases, IC50 values increased due to the presence of a detergent and the use of diverse enzyme concentrations, they were able to inhibit efficiently three unrelated enzymes, and IC50 values decreased under the influence of enzymeinhibitor pre-incubation.

Conclusion & Significance: Three out of the seven synthetized AR-inhibitors are not proposed to use as drugs due to their promiscuous nature, whereas the remaining four are worth further testing

Biography:

Dr. Patricia Hegger has completed her PhD on “Hyaluronan Based ECM-Mimetics with Tunable Charge Densities – Physico-Chemical Properties and Biological Implications” from Max-Planck-Institute for medical research in 2017. Before starting her career in industry she took over an interim-groupleader position at the Max-Planck-Institute for medical research continuing her studies on hyaluronic acid. She is now a labhead in the biopharmacy group of the TIDES Drug Product department of Sanofi-Aventis Deutschland GmbH, a global pharmaceutical company.

Abstract:

The uptake of subcutaneous (s.c.) administered formulations into the systemic circulation is a function of numerous quite diverse processes like active pharmaceutical ingredient (API) dissolution from the formulation and disintegration to monomers (“liberation”), local metabolism and the permeation through the interstitium and endothelium into the blood vessels (“absorption”). The determination of these parameters prior to launch of the drug is the field of biopharmacy, with its three pillars: In silico, in vitro and in vivo assessment combined with in vivo - in vitro correlation.

For s.c. administered formulations however there is only a limited number of systematically applied biopharmaceutical in vitro - in silico tools for characterization of those processes. For example the first in vitro methods for biopharmaceutical evaluation was published in 2015, whereas comparable methods for orally administered small molecules are established since the 1960s. Taken into account, that around 70 % of the marketed drugs today are s.c. applied, this is a highly evolving field with the potential of improvement for (I) molecule selection, (II) formulation selection and optimization and (III) understanding as well as prediction of in vivo findings in animals and humans.

Biography:

Annalisa Dalmoro graduated in Chemical Engineering, summa cum laude, in March 2009 at the University of Salerno (Italy), then she gained the Ph.D. degree in Science and Technologies for chemical, pharmaceutical and food industry in 2013. Starting from April 2013 she works as post-Doc researcher in TPP group (http://gruppotpp.unisa.it/en/) at the University of Salerno (Italy). Moreover, she is co-founder of the company Eng4Life srl, spin-off for technology transfer approved by the University of Salerno (http://www.eng4life.it/), established in January 2018. She has published about 40 research articles in international journals indexed on Scopus, WoS. She is also author of 2 patents..

Abstract:

Liposomes are the most versatile carriers for the delivery of a large variety of both lipophilic and hydrophilic drug molecules, being biocompatible and biodegradable. Despite their great advantages, their tendency to degrade and aggregate in biological fluids as well as in storage conditions drove the research towards new preparative approaches for liposomes stabilization, essentially based on superficial coatings or inclusion in polymeric materials. However the most used techniques, such as spraying, layering, sometimes by exploiting supercritical fluids, require complex and expensive apparatuses. Therefore, this work was developed with the idea to overcome typical liposomes stabilization limits, by choosing the consolidated wet granulation process as a method to obtain granules containing liposomes in a single step, by spraying on powder the liposomal suspension, previously produced by a novel continuous and rapid similmicrofluidic method. Literature highlights, although with only few works, the use of wet granulation as method to stabilize polymeric nanoparticles suspensions, by adding them in the binder phase. Instead, there are not experimental evidences about the use of liposomes suspensions as binder phase in wet granulation for both their stabilization and incorporation in pharmaceutical solid forms. Thus, this novel combination between wet granulation and the use of liposomes suspension spray as binder phase, allowed to reach both easy and cheap liposomes stabilization and the production of smart solid multiparticulate dosage forms, which could be ideal candidates for a combined fast/slow release of active ingredients, enhancers, fortifiers.

Biography:

Abstract:

Carnosine, an endogenous peptide, has been demonstrated to play an antitumorigenic role in certain types of cancer, suppressing glycolysis in cultured tumour cells^1,2. Recent evidence suggests that l-carnosine can interfere with oxidative phosphorylation as well³. However, its underlying mechanism is unclear.

The capsule of Karnozin EXTRA^® (Carnomed) is a unique patented formula of l-carnosine, in combination with vitamin E, coenzyme Q10, l-carnitine, northern blueberries extract and grape seed extract.

This food supplement was tested on two continuous cell lines with different energy pathways, MRC-5 (human embryo lung fibroblasts) and MCF-7 (human breast cancer cells), to evaluate its effects on mitochondrial respiration and certain mitochondrial respiratory chain complexes of the cells. Cells were treated for 24 hours with different concentrations of aqueous solution of the capsule Karnozin EXTRA^® (Carnomed) corresponding to concentrations of pure l-carnosine from the capsule of 2, 5, and 10 mM. Afterwards, we investigated basal respiration of intact cells and the activities of mitochondrial respiratory chain complexes I, II and IV. All measurements were performed using the Hansatech Oxygraph+ instrument (England).

The results showed that Karnozin EXTRA^® (Carnomed) exerted a significant reduction in the oxygen consumption in both cell lines in a dose-dependent manner. Moreover, the activities of mitochondrial electron transport chain complexes I, II and IV in both cell lines were compromised. The strongest inhibitory action was shown on the activity of complex II of mitochondrial electron transport chain.

The present study highlights a novel role of this capsule as a regulator of tested cells energy metabolism both in the anaerobic and aerobic pathways, which may give renewed impetus for its development as antitumor agent.

Biography:

Deepesh Lall has curiosity for the development and design of formulation which have much increased Bioavailability and optimistic rate of absorption. I am from starting wanted to overcome several disadvantage of conventional dosage form of Medicament, give an good outcome with novel drug delivery system specially Nanoparticles attracted more towards into NDDS. This Review plays an important role in the field of Pharmaceutic.

Abstract:

Ocular drug delivery still a challenging practice an attempt made to overcome the conventional dosage form with improving the Bioavailability and Concerning Therapeutic desired rate of Anterior Segment Delivery. Drug Delivery to the eye still a challenging practice to overcome  Nanoparticles incorporating for optimal Therapeutic activity, as drug molecules treated with the nanoparticles which help to cross from ocular barriers without causing permanent tissue damage. At present availability for the Ocular Anterior segment delivery the conventional dosage forms available with their limitations Bioavailability rate  for example solutions, suspensions and some ointments, while novel dosage forms playing important role for achieving more percentage of Bioavailability and rate of absorption without causing optical irritation, for example liposomes, nanoparticles, and implants. Aim of this work also come under the conclusion  80% to 90% of the available  formulations present in the market are conventional dosage forms, and they have limited bioavailability due to precorneal clearance and very short duration of action while novel drug delivery system  Nanoparticles possess advanced drug delivery medium. On study of certain literature review study conclusion found that major researcher is going with the development of sustained release and control release systems with higher precorneal Bioavailability. Such systems can improve the ocular bioavailability of drugs and provide high patient compliance. With going through several literature review study found   therapy into an eyes either by solutions, ointments dropping deteriorating by age, but nanoparticles like micelle, liposomes, Nano sponge’s and dendrimers hydrogel concluded efficient medium for chitosan, hyaluronic acids and antiglaucoma and these novel formulation have ability to deliver drugs in sustain and control release of medicaments. objective of this review is by using nanoparticles overcome the barriers of  Ocular Anterior segment delivery with increase and optimistic Bioavailability with crossing Ocular barriers.